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Recent Highlights in Targeted Protein Degradation

Drug Hunter

In Wednesday’s Flash Talk webinar , we covered recent highlights in targeted protein degradation, with lots of great questions from the audience. KT-333 and KT-003) AR degraders and ER degraders from Arvinas (bavdegalutamide/ARV-110, ARV-766, and ARV-471) MDM2 degraders from Kymera (e.g.

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Scientists generate new targeted protein degradation system that tunes a cell’s own proteins

Broad Institute

In one approach, they mark targeted proteins with “destroy me” tags that work with small molecules known as molecular glues to prompt the cell’s own protein-clearing machinery to gobble up the proteins. Liu is also a Howard Hughes Medical Institute investigator and a professor at Harvard University.

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Targeted protein degradation: turning undruggable targets into druggable targets

Drug Target Review

TPD is a rapidly evolving therapeutic modality to degrade a disease-causing proteins, thereby eliminating their function specifically. 1 TPD is expected to challenge undruggable proteins, which are highly difficult to target by conventional small molecules. How does TPD work?

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A covalent BTK ternary complex compatible with targeted protein degradation

Covalent Modifiers

Calabrese Nat Commun 14 , 1189, 2023 [link] Targeted protein degradation using heterobifunctional chimeras holds the potential to expand target space and grow the druggable proteome. Limiting this potential, however, is the remaining need to develop a ligand for the target of interest.

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€12 million raised for extracellular protein degradation research

Drug Discovery World

Biotechnology company Draupnir Bio has received equity investments totalling €12 million to support the company’s work in the field of targeted protein degradation (TPD).

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AI in Drug Discovery - A Highly Opinionated Literature Review (Part III)

Practical Cheminformatics

Property Prediction Machine Learning Methods for Small Data Challenges in Molecular Science [link] Practical guidelines for the use of gradient boosting for molecular property prediction [link] Application of message passing neural networks for molecular property prediction [link] Molecular Similarity Molecular Similarity: Theory, Applications, and (..)

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Discovery of a DCAF11-dependent cyanoacrylamide-containing covalent degrader of BET-proteins

Covalent Modifiers

Winter, Bioorganic & Medicinal Chemistry Letters , 2024 [link] Targeted protein degradation is mediated by small molecules that induce or stabilize proteinprotein interactions between targets and the ubiquitin–proteasome machinery. Gary Tin, Marko Cigler, Matthias Hinterndorfer, Kevin D.